Riociguat

Administration

Type: Vasodilator
Dosage Forms: Tab 0.5mg, 1mg, 1.5mg, 2mg, 2.5mg
Routes of Administration: Oral
Common Trade Names: Adempas

Adult Dosing

Chronic thromboembolic pulmonary HTN

0.5-2.5 mg PO TID

Pulmonary arterial hypertension

0.5-2.5 mg PO TID

Pediatric Dosing

Safety/efficacy not established in pediatric patients

Special Populations

Pregnancy Rating: X
Lactation risk: Avoid Use

Renal Dosing

Adult:
- CrCl >15: No adjustment
- CrCl <15: Not defined
Pediatric:
- Safety/efficacy not established in pediatric patients

Hepatic Dosing

Adult:
- Child-Pugh Class A or B: No adjustment
- Child-Pugh Class C: Not definied
Pediatric:
- Safety/efficacy not established in pediatric patients

Contraindications

Allergy to class/drug
Pregnancy
Breastfeeding
Pulmonary veno-occlusive disease
Idiopathic interstitial pneumonia

Adverse Reactions

Serious

Hemorrhage
Hemoptysis, severe
Hypotension, severe

Common

Headache, dizziness
Gastritis, dyspepsia, GERD
Nausea, diarrhea, vomiting, constipation
Hypotension
Anemia

Pharmacology

Half-life: 12h
Metabolism: Liver extensively; CYP450: 1A1 (primary), 2C8, 2J2, 3A4/5 substrate
Excretion: Urine 40% (6% unchanged); Feces 53% (15% unchanged)

Mechanism of Action

Sensitizes and stimulates binding of soluble guanylate cyclase to nitric oxide in nitric oxide-sGC-cGMP pathway
Increases cGMP production and subsequent vasodilation

Comments

See Also

References

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